scholarly journals Application of Asymmetrical Flow Field-Flow Fractionation for Characterizing the Size and Drug Release Kinetics of Theranostic Lipid Nanovesicles

2021 ◽  
Vol 22 (19) ◽  
pp. 10456
Author(s):  
Paulina Skupin-Mrugalska ◽  
Philipp A. Elvang ◽  
Martin Brandl
Keyword(s):  
Light Scattering ◽  
Flow Field ◽  
In Vitro Release ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Field Flow Fractionation ◽  
Liposome Size ◽  
Flow Fractionation ◽  
Vitro Release

Liposome size and in vitro release of the active substance belong to critical quality attributes of liposomal carriers. Here, we apply asymmetric flow field-flow fractionation (AF4) to characterize theranostic liposomes prepared by thin lipid film hydration/extrusion or microfluidics. The vesicles’ size was derived from multi-angle laser light scattering following fractionation (AF4) and compared to sizes derived from dynamic light scattering measurements. Additionally, we adapted a previously developed AF4 method to study zinc phthalocyanine (ZnPc) release/transfer from theranostic liposomes. To this end, theranostic liposomes were incubated with large acceptor liposomes serving as a sink (mimicking biological sinks) and were subsequently separated by AF4. During incubation, ZnPc was transferred from donor to acceptor fraction until reaching equilibrium. The process followed first-order kinetics with half-lives between 119.5–277.3 min, depending on the formulation. The release mechanism was postulated to represent a combination of Fickian diffusion and liposome relaxation. The rate constant of the transfer was proportional to the liposome size and inversely proportional to the ZnPc/POPC molar ratio. Our results confirm the usefulness of AF4 based method to study in vitro release/transfer of lipophilic payload, which may be useful to estimate the unwanted loss of drug from the liposomal carrier in vivo.

scholarly journals FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN

2021 ◽  
pp. 206-215
Author(s):  
DHARMENDER PALLERLA ◽  
SUMAN BANOTH ◽  
SUNKARI JYOTHI
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Release Studies ◽  
Swelling Studies ◽  
Vitro Release

Objective: The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies. Methods: The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and in vitro release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C. Results: FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. In vitro release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism. Conclusion: The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies.

scholarly journals Limitations of Nanoparticles Size Characterization by Asymmetric Flow Field‑Fractionation Coupled with Online Dynamic Light Scattering

2021 ◽  
Author(s):  
Francesco Giorgi ◽  
Judith M. Curran ◽  
Douglas Gilliland ◽  
Rita La Spina ◽  
Maurice Whelan ◽  
...  
Keyword(s):  
Light Scattering ◽  
Dynamic Light Scattering ◽  
Flow Field ◽  
Field Flow Fractionation ◽  
Asymmetric Flow ◽  
Uv Detector ◽  
Elution Time ◽  
On Line ◽  
Real Size ◽  
Flow Fractionation

AbstractThe development of reliable protocols suitable for the characterisation of the physical properties of nanoparticles in suspension is becoming crucial to assess the potential biological as well as toxicological impact of nanoparticles. Amongst sizing techniques, asymmetric flow field flow fractionation (AF4) coupled to online size detectors represents one of the most robust and flexible options to quantify the particle size distribution in suspension. However, size measurement uncertainties have been reported for on-line dynamic light scattering (DLS) detectors when coupled to AF4 systems. In this work we investigated the influence of the initial concentration of nanoparticles in suspension on the sizing capability of the asymmetric flow field-flow fractionation technique coupled with an on-line dynamic light scattering detector and a UV–Visible spectrophotometer (UV) detector. Experiments were performed with suspensions of gold nanoparticles with a nominal diameter of 40 nm and 60 nm at a range of particle concentrations. The results obtained demonstrate that at low concentration of nanoparticles, the AF4-DLS combined technique fails to evaluate the real size of nanoparticles in suspension, detecting an apparent and progressive size increase as a function of the elution time and of the concentration of nanoparticles in suspension.

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals Fast and Purification-Free Characterization of Bio-Nanoparticles in Biological Media by Electrical Asymmetrical Flow Field-Flow Fractionation Hyphenated with Multi-Angle Light Scattering and Nanoparticle Tracking Analysis Detection

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4703
Author(s):  
Roland Drexel ◽  
Agnieszka Siupa ◽  
Pauline Carnell-Morris ◽  
Michele Carboni ◽  
Jo Sullivan ◽  
...  
Keyword(s):  
Light Scattering ◽  
Flow Field ◽  
Chemical Characterization ◽  
Rabbit Serum ◽  
Field Flow Fractionation ◽  
Nanoparticle Tracking Analysis ◽  
Biological Media ◽  
Physico Chemical ◽  
Flow Fractionation

Accurate physico-chemical characterization of exosomes and liposomes in biological media is challenging due to the inherent complexity of the sample matrix. An appropriate purification step can significantly reduce matrix interferences, and thus facilitate analysis of such demanding samples. Electrical Asymmetrical Flow Field-Flow Fractionation (EAF4) provides online sample purification while simultaneously enabling access to size and Zeta potential of sample constituents in the size range of approx. 1–1000 nm. Hyphenation of EAF4 with Multi-Angle Light Scattering (MALS) and Nanoparticle Tracking Analysis (NTA) detection adds high resolution size and number concentration information turning this setup into a powerful analytical platform for the comprehensive physico-chemical characterization of such challenging samples. We here present EAF4-MALS hyphenated with NTA for the analysis of liposomes and exosomes in complex, biological media. Coupling of the two systems was realized using a flow splitter to deliver the sample at an appropriate flow speed for the NTA measurement. After a proof-of-concept study using polystyrene nanoparticles, the combined setup was successfully applied to analyze liposomes and exosomes spiked into cell culture medium and rabbit serum, respectively. Obtained results highlight the benefits of the EAF4-MALS-NTA platform to study the behavior of these promising drug delivery vesicles under in vivo like conditions.

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